Reaction Details |
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Target | Thyroid hormone receptor alpha |
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Ligand | BDBM18883 |
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Substrate/Competitor | BDBM18860 |
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Meas. Tech. | TRalpha-Binding Assay. |
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pH | 7±n/a |
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Temperature | 277.15±n/a K |
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IC50 | 1600±n/a nM |
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Citation | Koehler, K; Gordon, S; Brandt, P; Carlsson, B; Bäcksbro-Saeidi, A; Apelqvist, T; Agback, P; Grover, GJ; Nelson, W; Grynfarb, M; Färnegård, M; Rehnmark, S; Malm, J Thyroid receptor ligands. 6. A high affinity "direct antagonist" selective for the thyroid hormone receptor. J Med Chem49:6635-7 (2006) [PubMed] Article |
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More Info.: | Get all data from this article, Solution Info, Assay Method |
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Thyroid hormone receptor alpha |
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Name: | Thyroid hormone receptor alpha |
Synonyms: | C-erbA-alpha | EAR-7 | EAR7 | ERBA1 | NR1A1 | Nuclear receptor subfamily 1 group A member 1 | THA_HUMAN | THRA | THRA1 | THRA2 | Thyroid Hormone Receptor (TR-alpha) | Thyroid hormone receptor | Thyroid hormone receptor alpha | Thyroid hormone receptor apha | c-erbA-1 |
Type: | Receptor |
Mol. Mass.: | 54818.00 |
Organism: | Homo sapiens (Human) |
Description: | Recombinant hThR was obtained from nuclear extracts from SF9 cells infected with baculovirus vectors encoding for ThRalpha 1. |
Residue: | 490 |
Sequence: | MEQKPSKVECGSDPEENSARSPDGKRKRKNGQCSLKTSMSGYIPSYLDKDEQCVVCGDKA
TGYHYRCITCEGCKGFFRRTIQKNLHPTYSCKYDSCCVIDKITRNQCQLCRFKKCIAVGM
AMDLVLDDSKRVAKRKLIEQNRERRRKEEMIRSLQQRPEPTPEEWDLIHIATEAHRSTNA
QGSHWKQRRKFLPDDIGQSPIVSMPDGDKVDLEAFSEFTKIITPAITRVVDFAKKLPMFS
ELPCEDQIILLKGCCMEIMSLRAAVRYDPESDTLTLSGEMAVKREQLKNGGLGVVSDAIF
ELGKSLSAFNLDDTEVALLQAVLLMSTDRSGLLCVDKIEKSQEAYLLAFEHYVNHRKHNI
PHFWPKLLMKEREVQSSILYKGAAAEGRPGGSLGVHPEGQQLLGMHVVQGPQVRQLEQQL
GEAGSLQGPVLQHQSPKSPQQRLLELLHRSGILHARAVCGEDDSSEADSPSSSEEEPEVC
EDLAGNAASP
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BDBM18883 |
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BDBM18860 |
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Name | BDBM18883 |
Synonyms: | 3,5-dibromo-4-[4-hydroxy-3,5-bis(propan-2-yl)phenoxy]benzoic acid | JMC496635 Compound 3 | thyromimetic, 4 |
Type | Small organic molecule |
Emp. Form. | C19H20Br2O4 |
Mol. Mass. | 472.168 |
SMILES | CC(C)c1cc(Oc2c(Br)cc(cc2Br)C(O)=O)cc(C(C)C)c1O |
Structure |
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